口服姜黄素脂质体制备及其大鼠体内药动学考察

Preparation of curcumin liposomes and its oral pharmacokinetics in rats

目的制备卡波姆包衣姜黄素脂质体,并考察其在大鼠体内的药物动力学。方法采用薄膜分散法制备姜黄素脂质体,通过孵育法对姜黄素脂质体进行卡波姆包衣。采用微柱离心法测定姜黄素脂质体包衣前后包封率的变化。姜黄素脂质体大鼠口服给药后,以高效液相色谱(HPLC)法测定大鼠血浆中的药物浓度。结果脂质体包衣后包封率略有下降,姜黄素脂质体大鼠口服给药后药物动力学呈双室模型特征,相对生物利用度F(%)为281%,是普通脂质体的2.22倍。结论姜黄素脂质体经卡波姆包衣可明显提高姜黄素的口服生物利用度,药物峰浓度显著增加。

Objective To prepare Carbopol coated curcumin liposomes,and investigate its oral pharmacokinetics in rats.Methods After prepared by film dispersion method,curcumin liposomes were coated with carbopol. Then mini-column centrifugation method was adopted to determine the encapsulation efficiency （EE） before and after curcumin liposomes being coated. Drug concentration in rats plasma was detected by high performance lipid chromatography （HPLC） after curcumin liposomes administered to rats.Results The EE of curcumin liposomes decreased slightly after coated. Carbopol coated curcumin liposomes after oral administration in rats showed two-compartment model pharmacokinetic characteristics,and the relative bioavailability F（%） was 281%,which was 2.22 times as the non-coated curcumin liposomes.Conclusion After coated by carbopol,the oral bioavailability of curcumin liposomes can be significantly improved,and the maximum drug concentration also increased.